中国药物警戒 ›› 2014, Vol. 11 ›› Issue (10): 596-600.

• 质量与工艺研究 • 上一篇    下一篇

瑞舒伐他汀钙片溶出度研究

蔡垠, 苗艳, 武利, 周志亮*, 朱金莲, 申晓凤   

  1. 润泽制药苏州有限公司,江苏 苏州 215126
  • 收稿日期:2014-01-06 修回日期:2016-02-03 出版日期:2014-10-08 发布日期:2016-03-02
  • 通讯作者: 周志亮,男,博士,药物制剂研发。
  • 作者简介:蔡垠,女,硕士,工程师,药物制剂研发。

Research on the Dissolution Profiles of Rosuvastatin Calcium Tablets

CAI Yin, MIAO Yan, WU Li, ZHOU Zhi-liang*, ZHU Jin-lian, SHEN Xiao-feng   

  1. Runze Pharmaceuticals (Suzhou) CO., LTD., Jiangsu Suzhou 215126, China
  • Received:2014-01-06 Revised:2016-02-03 Online:2014-10-08 Published:2016-03-02

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摘要： 目的建立瑞舒伐他汀钙片溶出度研究方法。方法HPLC法,色谱柱：Agilent Extend C18（4.6×250 mm,5 μm）;流动相：以乙腈为流动相A,以0.02%三氟乙酸溶液为流动相B,0~13 min,A：37%,13~27 min,A：37%~90%;检测波长：242 nm;流速：1.0 mL·min-1;发生降解行为的溶出度样品经碱中和前处理后以瑞舒伐他汀钙与瑞舒伐他汀非对映异构体峰面积之和计算累积溶出量（%）。结果瑞舒伐他汀钙在pH 1.0盐酸溶液不稳定,降解生成瑞舒伐他汀非对映异构体,瑞舒伐他汀-5S-内酯和瑞舒伐他汀-5R-内酯,后两者经碱中和处理后重新生成瑞舒伐他汀及瑞舒伐他汀非对映异构体,且瑞舒伐他汀钙片在pH 1.0盐酸溶液中溶出速率最慢。结论瑞舒伐他汀钙在pH 1.0盐酸溶液中溶出曲线可作为处方筛选的依据。

关键词: 瑞舒伐他汀钙, 瑞舒伐他汀钙非对映异构体, 溶出度, 累积溶出量（%）, 校正因子

Abstract: ObjectiveTo establish the dissolution method of rosuvastatin calcium tablets. MethodsColumn: Agilent Extend C18 (4.6×250 mm, 5 μm), eluted with acetonitrile and 0.02% TFA in gradient mode. The ratio of acetonitrile kept 37% in 13 min and increased to 90% from 13~27 min at a flow rate of 1.0 mL·min-1 when the detective wavelength was set at 242 nm, plus the rosuvastatin and (3S, 5S)-rosuvastatin calcium peak area to calculate the cumulative release amount (%). ResultsRosuvastatin calcium was instabile in pH 1.0 hydrochloric acid solution and degraded to (3S, 5S)-rosuvastatin calcium, rosuvastatin-5S-lactone and rosuvastatin-5R-lactone, when treated with alkali and regenerated to rosuvastatin and (3S, 5S)-Rosuvastatin calcium, also the dissolution profile of rosuvastatin calcium tablets in pH1.0 hydrochloric acid solution was the slowest one. ConclusionThe dissolution profile of rosuvastatin calcium tablets in pH 1.0 hydrochloric acid solution can be used as the basis for formulation screening.

Key words: rosuvastatin calcium, (3S, 5S)-rosuvastatin calcium, dissolution, cumulative release amount (%), correction factor

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